- COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
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Paragraph 0472-0477
(2018/04/20)
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- New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase
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Herein, we described a new class of uncharged non-pyridinium reactivators for nerve agent-inhibited acetylcholinesterase (AChE). Based on a dual site binding strategy, we conjugated the imidazolium aldoxime to different peripheral site ligands (PSLs) of A
- Wei, Zhao,Liu, Yan-Qin,Zhou, Xin-Bo,Luo, Yuan,Huang, Chun-Qian,Wang, Yong-An,Zheng, Zhi-Bing,Li, Song
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supporting information
p. 5743 - 5748
(2015/01/09)
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- Synthesis of δ- And ε-cyanoesters by zinc-catalyzed ring-opening of cyclic ethers with acid chlorides and subsequent cyanation
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In the present study, the zinc-catalyzed cleavage of cyclic ethers with acid halides as nucleophiles to yield chloroesters with different chain length has been investigated in detail. In the presence of straightforward and commercially available zinc salts as pre-catalysts excellent yields and selectivities were feasible. After studying the reaction conditions and the scope of the method, several efforts were carried out to understand the reaction mechanism. The obtained chloroesters were subsequently converted to δ- and ε-cyano esters, which are useful precursors in natural product synthesis. Graphical Abstract: [Figure not available: see fulltext.]
- Enthaler, Stephan,Weidauer, Maik
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experimental part
p. 168 - 175
(2012/03/27)
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- Copper-catalyzed cross-coupling reaction of organoboron compounds with primary alkyl halides and pseudohalides
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Non-activated alkyl electrophiles, including alkyl iodides, bromides, tosylates, mesylates, and even chlorides, underwent copper-catalyzed cross-coupling with aryl boron compounds and alkyl 9-BBN reagents (see scheme; 9-BBN=9-borabicyclo[3.3.1]nonane). The reactions proceed with practically useful reactivities and thus complement palladium- and nickel-catalyzed Suzuki-Miyaura coupling reactions of alkyl halides.
- Yang, Chu-Ting,Zhang, Zhen-Qi,Liu, Yu-Chen,Liu, Lei
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supporting information; experimental part
p. 3904 - 3907
(2011/05/15)
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- Single-pot conversion of an acid to the corresponding 4-chlorobutyl ester
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A single pot conversion of carboxylic acids into the corresponding 4-chlorobutyl esters has been achieved by a novel procedure. The intermediate acid chlorides are not isolated. The double bond and aromatic methoxy group survive the mild reaction conditions. In almost all the examples studied the products are purified by simple flash chromatography.
- Pal, Sutanuka,Pal, Sudhir Chandra
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p. 596 - 599
(2012/04/18)
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- Agonistic activity and charge driven interaction potentiality of PAF derivatives
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Taking into account the contribution of the C2 substituent to the interaction ability of PAF derivatives, an investigation has been undertaken on: i) the role of the presence of two unitary charges of opposite sign in the molecule; ii) the role
- Villa,Pallavicini,Villa,Valoti,Ferri,Berti
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p. 1379 - 1399
(2007/10/02)
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- 3- and 4-biphenyloxyaminoalkanes and related compounds as anti-inflammatory and analgetic agents
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Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3; b is an integer of 0-2; n is an integer of 3-12; each X and each Y are independently -halo, --R1, -alkoxy, or -phenyl; and B is selected from the group consisting of: --NR1 R2, --NR1 (CH2 CH2 OH), STR2 in which R1 and R2 are independently H, alkyl or cycloalkyl; R3 is H, alkyl or --CH2 CH2 OH; and m is an integer of 3-8. Novel compounds are those wherein n is at least 6 if both a and b are 0.
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- Anti-inflammatory guanidines
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A compound having the formula STR1 where Ar=naphthyl, biphenyl, or quinolinyl; X=oxygen or NH; Y=2 to 8; R1 =phenyl, substituted phenyl, hydrogen, lower alkyl; and R2 is the same or different from R3 and is alkyl, cycloalkyl, phenyl, substituted phenyl, thiazolyl; and the pharmaceutically acceptable salts thereof. Compounds of this general formula are useful as anti-inflammatories, and as anti-psoriatic agents.
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